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Călin-Aurel Drăgan, Rolf W. Hartmann & Matthias Bureik. (2006) A fission yeast-based test system for the determination of IC50 values of anti-prostate tumor drugs acting on CYP21. Journal of Enzyme Inhibition and Medicinal Chemistry 21:5, pages 547-556.
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Tomasz M. Wróbel, Flemming Steen Jørgensen, Amit V. Pandey, Angelika Grudzińska, Katyayani Sharma, Jibira Yakubu & Fredrik Björkling. (2023) Non-steroidal CYP17A1 Inhibitors: Discovery and Assessment. Journal of Medicinal Chemistry 66:10, pages 6542-6566.
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Faheimeh Haghbeen, Nargess Ghorbanian, Golnaz Hajatpour, Javad Zamani Amirzakaria, Hossein Eshghi & Kamahldin Haghbeen. (2021) Introducing a potential lead structure for the synthesis of more specific inhibitors of tyrosinases and catechol oxidases. Journal of the Iranian Chemical Society 19:4, pages 1385-1396.
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Nicolas Lebouvier, Fabrice Pagniez, Young Min Na, Da Shi, Patricia Pinson, Mathieu Marchivie, Jean Guillon, Tarek Hakki, Rita Bernhardt, Sook Wah Yee, Claire Simons, Marie-Pierre Lézé, Rolf W. Hartmann, Angélique Mularoni, Guillaume Le Baut, Isabelle Krimm, Ruben Abagyan, Patrice Le Pape & Marc Le Borgne. (2020) Synthesis, Optimization, Antifungal Activity, Selectivity, and CYP51 Binding of New 2-Aryl-3-azolyl-1-indolyl-propan-2-ols. Pharmaceuticals 13:8, pages 186.
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Katharina R. Beck, Lucija Telisman, Chris J. van Koppen, George R. ThompsonIIIIII & Alex Odermatt. (2020) Molecular mechanisms of posaconazole- and itraconazole-induced pseudohyperaldosteronism and assessment of other systemically used azole antifungals. The Journal of Steroid Biochemistry and Molecular Biology 199, pages 105605.
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Melanie Patt, Katharina R. Beck, Tobias Di Marco, Marie-Christin Jäger, Victor González-Ruiz, Julien Boccard, Serge Rudaz, Rolf W. Hartmann, Mohamed Salah, Chris J. van Koppen, Matthias Grill & Alex Odermatt. (2020) Profiling of anabolic androgenic steroids and selective androgen receptor modulators for interference with adrenal steroidogenesis. Biochemical Pharmacology 172, pages 113781.
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Muhammad Akram, Melanie Patt, Teresa Kaserer, Veronika Temml, Watcharee Waratchareeyakul, Denise V. Kratschmar, Joerg Haupenthal, Rolf W. Hartmann, Alex Odermatt & Daniela Schuster. (2019) Identification of the fungicide epoxiconazole by virtual screening and biological assessment as inhibitor of human 11β-hydroxylase and aldosterone synthase. The Journal of Steroid Biochemistry and Molecular Biology 192, pages 105358.
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Silvia Gobbi, Qingzhong Hu, Giacomo Foschi, Elena Catanzaro, Federica Belluti, Angela Rampa, Carmela Fimognari, Rolf W. Hartmann & Alessandra Bisi. (2019) Benzophenones as xanthone-open model CYP11B1 inhibitors potentially useful for promoting wound healing. Bioorganic Chemistry 86, pages 401-409.
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Julie Islin, Cecilie Hurup Munkboel & Bjarne Styrishave. (2018) Steroidogenic disruptive effects of the serotonin-noradrenaline reuptake inhibitors duloxetine, venlafaxine and tramadol in the H295R cell assay and in a recombinant CYP17 assay. Toxicology in Vitro 47, pages 63-71.
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Juliette Emmerich, Chris J. van Koppen, Jens L. Burkhart, Roger T. Engeli, Qingzhong Hu, Alex Odermatt & Rolf W. Hartmann. (2018) Accelerated skin wound healing by selective 11β-Hydroxylase (CYP11B1) inhibitors. European Journal of Medicinal Chemistry 143, pages 591-597.
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Juliette Emmerich, Chris J. van Koppen, Jens L. Burkhart, Qingzhong Hu, Lorenz Siebenbürger, Carsten Boerger, Claudia Scheuer, Matthias W. Laschke, Michael D. Menger & Rolf W. Hartmann. (2017) Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing’s Disease. Journal of Medicinal Chemistry 60:12, pages 5086-5098.
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Silvia Gobbi, Qingzhong Hu, Christina Zimmer, Federica Belluti, Angela Rampa, Rolf W. Hartmann & Alessandra Bisi. (2016) Targeting Steroidogenic Cytochromes P450 (CYPs) with 6-Substituted 1-Imidazolylmethylxanthones. ChemMedChem 11:16, pages 1770-1777.
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Silvia Gobbi, Qingzhong Hu, Christina Zimmer, Matthias Engel, Federica Belluti, Angela Rampa, Rolf W. Hartmann & Alessandra Bisi. (2016) Exploiting the Chromone Scaffold for the Development of Inhibitors of Corticosteroid Biosynthesis. Journal of Medicinal Chemistry 59:6, pages 2468-2477.
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Najim A. Al-Masoudi, Nabeel A. Abdul-Rida, Rawaa A. Kadhim, Sebastian J. Krug, Matthias Engel & Bahjat A. Saeed. (2015) Synthesis and CYP17α hydroxylase inhibition activity of new 3α- and 3β-ester derivatives of pregnenolone and related ether analogues. Medicinal Chemistry Research 25:2, pages 310-321.
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Najim A. Al-Masoudi, Rawaa A. Kadhim, Nabeel A. Abdul-Rida, Bahjat A. Saeed & Matthias Engel. (2015) New biaryl-chalcone derivatives of pregnenolone via Suzuki–Miyaura cross-coupling reaction. Synthesis, CYP17 hydroxylase inhibition activity, QSAR, and molecular docking study. Steroids 101, pages 43-50.
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Najim A. Al-Masoudi, Kuthiar M. Mahdi, Nabeel A. Abdul-Rida, Bahjat A. Saeed & Mathias Engel. (2015) A new pregnenolone analogues as privileged scaffolds in inhibition of CYP17 hydroxylase enzyme. Synthesis and in silico molecular docking study. Steroids 100, pages 52-59.
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Qingzhong Hu, Lina Yin, Amjad Ali, Andrew J. Cooke, Jonathan Bennett, Paul Ratcliffe, Michael Man-Chu Lo, Edward Metzger, Scott Hoyt & Rolf W. Hartmann. (2015)
Novel Pyridyl Substituted 4,5-Dihydro-[1,2,4]triazolo[4,3-
a
]quinolines as Potent and Selective Aldosterone Synthase Inhibitors with Improved in Vitro Metabolic Stability
. Journal of Medicinal Chemistry 58:5, pages 2530-2537.
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Najim A. Al-Masoudi, Dawood S. Ali, Bahjat Saeed, Rolf W. Hartmann, Matthias Engel, Sajid Rashid & Aamer Saeed. (2014) New CYP17 Hydroxylase Inhibitors: Synthesis, Biological Evaluation, QSAR, and Molecular Docking Study of New Pregnenolone Analogs. Archiv der Pharmazie 347:12, pages 896-907.
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Lina Yin, Qingzhong Hu, Juliette Emmerich, Michael Man-Chu Lo, Edward Metzger, Amjad Ali & Rolf W. Hartmann. (2014) Novel Pyridyl- or Isoquinolinyl-Substituted Indolines and Indoles as Potent and Selective Aldosterone Synthase Inhibitors. Journal of Medicinal Chemistry 57:12, pages 5179-5189.
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Qingzhong Hu & Rolf W. Hartmann. 2014. Cancer Drug Design and Discovery. Cancer Drug Design and Discovery
319
356
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Maria Grazia Ferlin, Davide Carta, Roberta Bortolozzi, Razieh Ghodsi, Adele Chimento, Vincenzo Pezzi, Stefano Moro, Nina Hanke, Rolf W. Hartmann, Giuseppe Basso & Giampietro Viola. (2013) Design, Synthesis, and Structure–Activity Relationships of Azolylmethylpyrroloquinolines as Nonsteroidal Aromatase Inhibitors. Journal of Medicinal Chemistry 56:19, pages 7536-7551.
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Juliette Emmerich, Qingzhong Hu, Nina Hanke & Rolf W. Hartmann. (2013) Cushing’s Syndrome: Development of Highly Potent and Selective CYP11B1 Inhibitors of the (Pyridylmethyl)pyridine Type. Journal of Medicinal Chemistry 56:15, pages 6022-6032.
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Sebastian J. Krug, Qingzhong Hu & Rolf W. Hartmann. (2013) Hits identified in library screening demonstrate selective CYP17A1 lyase inhibition. The Journal of Steroid Biochemistry and Molecular Biology 134, pages 75-79.
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Silvia Gobbi, Qingzhong Hu, Matthias Negri, Christina Zimmer, Federica Belluti, Angela Rampa, Rolf W. Hartmann & Alessandra Bisi. (2013) Modulation of Cytochromes P450 with Xanthone-Based Molecules: From Aromatase to Aldosterone Synthase and Steroid 11β-Hydroxylase Inhibition. Journal of Medicinal Chemistry 56:4, pages 1723-1729.
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Lina Yin, Qingzhong Hu & Rolf W. Hartmann. (2013) Tetrahydropyrroloquinolinone Type Dual Inhibitors of Aromatase/Aldosterone Synthase as a Novel Strategy for Breast Cancer Patients with Elevated Cardiovascular Risks. Journal of Medicinal Chemistry 56:2, pages 460-470.
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Qingzhong Hu, Lina Yin & Rolf W. Hartmann. (2012) Selective Dual Inhibitors of CYP19 and CYP11B2: Targeting Cardiovascular Diseases Hiding in the Shadow of Breast Cancer. Journal of Medicinal Chemistry 55:16, pages 7080-7089.
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Natasha M. DeVore & Emily E. Scott. (2012) Structures of cytochrome P450 17A1 with prostate cancer drugs abiraterone and TOK-001. Nature 482:7383, pages 116-119.
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Yaseen A. Al-Soud, Michael Heydel & Rolf W. Hartmann. (2011) Design and synthesis of 1,3,5-trisubstituted 1,2,4-triazoles as CYP enzyme inhibitors. Tetrahedron Letters 52:48, pages 6372-6375.
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Tomohiro Kaku, Takenori Hitaka, Akio Ojida, Nobuyuki Matsunaga, Mari Adachi, Toshimasa Tanaka, Takahito Hara, Masuo Yamaoka, Masami Kusaka, Teruaki Okuda, Satoru Asahi, Shuichi Furuya & Akihiro Tasaka. (2011) Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer. Bioorganic & Medicinal Chemistry 19:21, pages 6383-6399.
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Ulrike E. Hille, Christina Zimmer, Jörg Haupenthal & Rolf W. Hartmann. (2011) Optimization of the First Selective Steroid-11β-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases. ACS Medicinal Chemistry Letters 2:8, pages 559-564.
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Simon Lucas, Matthias Negri, Ralf Heim, Christina Zimmer & Rolf W. Hartmann. (2011)
Fine-Tuning the Selectivity of Aldosterone Synthase Inhibitors: Structure−Activity and Structure−Selectivity Insights from Studies of Heteroaryl Substituted 1,2,5,6-Tetrahydropyrrolo[3,2,1-
ij
]quinolin-4-one Derivatives
. Journal of Medicinal Chemistry 54:7, pages 2307-2319.
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Tomohiro Kaku, Saori Tsujimoto, Nobuyuki Matsunaga, Toshimasa Tanaka, Takahito Hara, Masuo Yamaoka, Masami Kusaka & Akihiro Tasaka. (2011) 17,20-Lyase inhibitors. Part 3: Design, synthesis, and structure–activity relationships of biphenylylmethylimidazole derivatives as novel 17,20-lyase inhibitors. Bioorganic & Medicinal Chemistry 19:7, pages 2428-2442.
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Angela Stefanachi, Angelo D. Favia, Orazio Nicolotti, Francesco Leonetti, Leonardo Pisani, Marco Catto, Christina Zimmer, Rolf W. Hartmann & Angelo Carotti. (2011) Design, Synthesis, and Biological Evaluation of Imidazolyl Derivatives of 4,7-Disubstituted Coumarins as Aromatase Inhibitors Selective over 17-α-Hydroxylase/C17−20 Lyase. Journal of Medicinal Chemistry 54:6, pages 1613-1625.
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V. V. Shumyantseva, T. V. Bulko, A. Yu. Misharin & A. I. Archakov. (2011) Screening of potential substrates or inhibitors of cytochrome P450 17A1 (CYP17A1) by electrochemical methods. Biochemistry (Moscow) Supplement Series B: Biomedical Chemistry 5:1, pages 55-59.
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Tomohiro Kaku, Nobuyuki Matsunaga, Akio Ojida, Toshimasa Tanaka, Takahito Hara, Masuo Yamaoka, Masami Kusaka & Akihiro Tasaka. (2011) 17,20-Lyase inhibitors. Part 4: Design, synthesis and structure–activity relationships of naphthylmethylimidazole derivatives as novel 17,20-lyase inhibitors. Bioorganic & Medicinal Chemistry 19:5, pages 1751-1770.
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Ulrike E. Hille, Christina Zimmer, Carsten A. Vock & Rolf W. Hartmann. (2010) First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases. ACS Medicinal Chemistry Letters 2:1, pages 2-6.
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Štefan Starčević, Petra Brožič, Samo Turk, Jožko Cesar, Tea Lanišnik Rižner & Stanislav Gobec. (2010) Synthesis and Biological Evaluation of (6- and 7-Phenyl) Coumarin Derivatives as Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1. Journal of Medicinal Chemistry 54:1, pages 248-261.
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Christina Zimmer, Marieke Hafner, Michael Zender, Dominic Ammann, Rolf W. Hartmann & Carsten A. Vock. (2011) N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2). Bioorganic & Medicinal Chemistry Letters 21:1, pages 186-190.
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Qingzhong Hu, Carsten Jagusch, Ulrike E. Hille, Jörg Haupenthal & Rolf W. Hartmann. (2010) Replacement of Imidazolyl by Pyridyl in Biphenylmethylenes Results in Selective CYP17 and Dual CYP17/CYP11B1 Inhibitors for the Treatment of Prostate Cancer. Journal of Medicinal Chemistry 53:15, pages 5749-5758.
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Silvia Gobbi, Christina Zimmer, Federica Belluti, Angela Rampa, Rolf W. Hartmann, Maurizio Recanatini & Alessandra Bisi. (2010) Novel Highly Potent and Selective Nonsteroidal Aromatase Inhibitors: Synthesis, Biological Evaluation and Structure−Activity Relationships Investigation. Journal of Medicinal Chemistry 53:14, pages 5347-5351.
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Qingzhong Hu, Lina Yin, Carsten Jagusch, Ulrike E. Hille & Rolf W. Hartmann. (2010) Isopropylidene Substitution Increases Activity and Selectivity of Biphenylmethylene 4-Pyridine Type CYP17 Inhibitors. Journal of Medicinal Chemistry 53:13, pages 5049-5053.
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Qingzhong Hu, Matthias Negri, Sureyya Olgen & Rolf W. Hartmann. (2010) The Role of Fluorine Substitution in Biphenyl Methylene Imidazole-Type CYP17 Inhibitors for the Treatment of Prostate Carcinoma. ChemMedChem 5:6, pages 899-910.
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Simon Lucas, Ralf Heim, Christina Ries, Katarzyna E. Schewe, Barbara Birk & Rolf W. Hartmann. (2008)
In Vivo Active Aldosterone Synthase Inhibitors with Improved Selectivity: Lead Optimization Providing a Series of Pyridine Substituted 3,4-Dihydro-1
H
-quinolin-2-one Derivatives
. Journal of Medicinal Chemistry 51:24, pages 8077-8087.
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Simon Lucas, Ralf Heim, Matthias Negri, Iris Antes, Christina Ries, Katarzyna E. Schewe, Alessandra Bisi, Silvia Gobbi & Rolf W. Hartmann. (2008) Novel Aldosterone Synthase Inhibitors with Extended Carbocyclic Skeleton by a Combined Ligand-Based and Structure-Based Drug Design Approach. Journal of Medicinal Chemistry 51:19, pages 6138-6149.
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Mariano A. E. Pinto‐Bazurco Mendieta, Matthias Negri, Qingzhong Hu, Ulrike E. Hille, Carsten Jagusch, Kerstin Jahn‐Hoffmann, Ursula Müller‐Vieira, Dirk Schmidt, Thomas Lauterbach & Rolf W. Hartmann. (2008) CYP17 Inhibitors. Annulations of Additional Rings in Methylene Imidazole Substituted Biphenyls: Synthesis, Biological Evaluation and Molecular Modelling. Archiv der Pharmazie 341:10, pages 597-609.
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Sabrina Castellano, Giorgio Stefancich, Rino Ragno, Katarzyna Schewe, Marisabella Santoriello, Antonia Caroli, Rolf W. Hartmann & Gianluca Sbardella. (2008) CYP19 (aromatase): Exploring the scaffold flexibility for novel selective inhibitors. Bioorganic & Medicinal Chemistry 16:18, pages 8349-8358.
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Ralf Heim, Simon Lucas, Cornelia M. Grombein, Christina Ries, Katarzyna E. Schewe, Matthias Negri, Barbara Birk & Rolf W. Hartmann. (2008) Overcoming Undesirable CYP1A2 Inhibition of Pyridylnaphthalene-Type Aldosterone Synthase Inhibitors: Influence of Heteroaryl Derivatization on Potency and Selectivity. Journal of Medicinal Chemistry 51:16, pages 5064-5074.
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Mariano A. E. Pinto-Bazurco Mendieta, Matthias Negri, Carsten Jagusch, Ursula Müller-Vieira, Thomas Lauterbach & Rolf W. Hartmann. (2008) Synthesis, Biological Evaluation, and Molecular Modeling of Abiraterone Analogues: Novel CYP17 Inhibitors for the Treatment of Prostate Cancer. Journal of Medicinal Chemistry 51:16, pages 5009-5018.
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Marie-Pierre Lézé, Anja Palusczak, Rolf W. Hartmann & Marc Le Borgne. (2008) Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors. Bioorganic & Medicinal Chemistry Letters 18:16, pages 4713-4715.
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Qingzhong Hu, Matthias Negri, Kerstin Jahn-Hoffmann, Yan Zhuang, Sureyya Olgen, Marc Bartels, Ursula Müller-Vieira, Thomas Lauterbach & Rolf W. Hartmann. (2008) Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17α-hydroxylase-17,20-lyase (CYP17)—Part II: Core rigidification and influence of substituents at the methylene bridge. Bioorganic & Medicinal Chemistry 16:16, pages 7715-7727.
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Mariano A.E. Pinto-Bazurco Mendieta, Matthias Negri, Carsten Jagusch, Ulrike E. Hille, Ursula Müller-Vieira, Dirk Schmidt, Klaus Hansen & Rolf W. Hartmann. (2008) Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17. Bioorganic & Medicinal Chemistry Letters 18:1, pages 267-273.
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Silvia Gobbi, Andrea Cavalli, Matthias Negri, Katarzyna E. Schewe, Federica Belluti, Lorna Piazzi, Rolf W. Hartmann, Maurizio Recanatini & Alessandra Bisi. (2007) Imidazolylmethylbenzophenones as Highly Potent Aromatase Inhibitors. Journal of Medicinal Chemistry 50:15, pages 3420-3422.
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Tarek Hakki & Rita Bernhardt. (2006) CYP17- and CYP11B-dependent steroid hydroxylases as drug development targets. Pharmacology & Therapeutics 111:1, pages 27-52.
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Daniela Schuster, Christian Laggner, Theodora M. Steindl, Anja Palusczak, Rolf W. Hartmann & Thierry Langer. (2006) Pharmacophore Modeling and in Silico Screening for New P450 19 (Aromatase) Inhibitors. Journal of Chemical Information and Modeling 46:3, pages 1301-1311.
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Marieke Voets, Iris Antes, Christiane Scherer, Ursula Müller-Vieira, Klaus Biemel, Sandrine Marchais-Oberwinkler & Rolf W. Hartmann. (2006) Synthesis and Evaluation of Heteroaryl-Substituted Dihydronaphthalenes and Indenes: Potent and Selective Inhibitors of Aldosterone Synthase (CYP11B2) for the Treatment of Congestive Heart Failure and Myocardial Fibrosis. Journal of Medicinal Chemistry 49:7, pages 2222-2231.
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Marie-Pierre Lézé, Marc Le Borgne, Patricia Pinson, Anja Palusczak, Muriel Duflos, Guillaume Le Baut & Rolf W. Hartmann. (2006) Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: Potent and selective aromatase inhibitors. Bioorganic & Medicinal Chemistry Letters 16:5, pages 1134-1137.
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Andrea Cavalli, Alessandra Bisi, Carlo Bertucci, Carlo Rosini, Anja Paluszcak, Silvia Gobbi, Egidio Giorgio, Angela Rampa, Federica Belluti, Lorna Piazzi, Piero Valenti, Rolf W. Hartmann & Maurizio Recanatini. (2005) Enantioselective Nonsteroidal Aromatase Inhibitors Identified through a Multidisciplinary Medicinal Chemistry Approach. Journal of Medicinal Chemistry 48:23, pages 7282-7289.
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Marieke Voets, Iris Antes, Christiane Scherer, Ursula Müller-Vieira, Klaus Biemel, Catherine Barassin, Sandrine Marchais-Oberwinkler & Rolf W. Hartmann. (2005) Heteroaryl-Substituted Naphthalenes and Structurally Modified Derivatives: Selective Inhibitors of CYP11B2 for the Treatment of Congestive Heart Failure and Myocardial Fibrosis. Journal of Medicinal Chemistry 48:21, pages 6632-6642.
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Sarah Ulmschneider, Ursula Müller-Vieira, Markus Mitrenga, Rolf W. Hartmann, Sandrine Oberwinkler-Marchais, Christian D. Klein, Matthias Bureik, Rita Bernhardt, Iris Antes & Thomas Lengauer. (2004) Synthesis and Evaluation of Imidazolylmethylenetetrahydronaphthalenes and Imidazolylmethyleneindanes: Potent Inhibitors of Aldosterone Synthase. Journal of Medicinal Chemistry 48:6, pages 1796-1805.
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Sarah Ulmschneider, Ursula Müller-Vieira, Christian D. Klein, Iris Antes, Thomas Lengauer & Rolf W. Hartmann. (2005) Synthesis and Evaluation of (Pyridylmethylene)tetrahydronaphthalenes/-indanes and Structurally Modified Derivatives: Potent and Selective Inhibitors of Aldosterone Synthase. Journal of Medicinal Chemistry 48:5, pages 1563-1575.
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